1-Hydroxybenzotriazole → Tert-butyl 2-[3-{1-(4-sulfamoylphenyl)-5-p-tolyl-1h-pyrazol-3-yl}propanamido]ethylcarbamate

HRID 16656

反応式

HRID 16656 の反応式
[CH3:1][C:2]1[CH:7]=[CH:6][C:5]([C:8]2[N:12]([C:13]3[CH:18]=[CH:17][C:16]([S:19]([NH2:22])(=[O:21])=[O:20])=[CH:15][CH:14]=3)[N:11]=[C:10]([C:23](F)(F)F)[CH:9]=2)=[CH:4][CH:3]=1.C1CN2C3C(CCC2)=C2[O:46][C:45]4C(C=C5C6[C:44]=4CCC[N+]=6CCC5)=C(C4C=CC(S(Cl)(=O)=O)=CC=4S([O-])(=O)=O)C2=CC=3C1.[NH2:69][CH2:70][CH2:71][NH:72][C:73](=[O:79])[O:74][C:75]([CH3:78])([CH3:77])[CH3:76].Cl.C(N=C=NCCCN(C)C)C.ON1C2C=CC=CC=2N=N1.C(N(CC)C(C)C)(C)C>CN(C=O)C>[S:19]([C:16]1[CH:17]=[CH:18][C:13]([N:12]2[C:8]([C:5]3[CH:6]=[CH:7][C:2]([CH3:1])=[CH:3][CH:4]=3)=[CH:9][C:10]([CH2:23][CH2:44][C:45]([NH:69][CH2:70][CH2:71][NH:72][C:73](=[O:79])[O:74][C:75]([CH3:76])([CH3:78])[CH3:77])=[O:46])=[N:11]2)=[CH:14][CH:15]=1)(=[O:20])(=[O:21])[NH2:22]

参加物

7

実験手順

a Celecox-Sulforhodamine Analog: Compound 30f was synthesized by the method outlined in FIG. 3. Briefly, Compound 30c as synthesized as set forth hereinabove. Compound 30c was then complexed with tert-butyl 2-aminoethylcarbamate for 16 hours at room temperature in the presence of 1-ethyl-3-(3′-dimethylaminopropyl)carbodiimide hydrochloride (EDCl), 1-hydroxybenzotriazole (HOBt), and N,N-diisopropylethylamine (DIPEA) in mimethylformamide (DMF) to produce tert-butyl 2-[3-{1-(4-sulfamoylphenyl)-5-p-tolyl-1H-pyrazol-3-yl}propanamido]ethylcarbamate as a yellow solid (46% yield). This product was then dissolved in dichloromethane and treated with HCl (gas) for 2 hours at room temperature, producing N-(2-aminoethyl)-3-{1-(4-sulfamoylphenyl)-5-p-tolyl-1H-pyrazol-3-yl}propanamide hydrochloride as a yellow solid (80% yield).

出典と根拠

ORDレコード
ord-de5eb08e7d1e4c42908d8980e52fde1c
出典データセット
uspto-grants-2010_06
特許番号
US07736624B2

関連ノート

読み込み中…